Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore - 570 006, Karnataka, India.
Eur J Med Chem. 2013 Feb;60:325-32. doi: 10.1016/j.ejmech.2012.12.029. Epub 2012 Dec 20.
Synthesis of a new series of urea/thiourea derivatives of Gly/Pro conjugated benzisoxazole has been reported. Structure of the compounds was characterized by physical and spectroscopical data and has been screened for their in vitro antiglycation activity. Several compounds showed promising activity with IC(50) < 5 μM compared to standard rutin (IC(50) = 41.9 μM). Further, it was found that compounds containing methoxy and bromine substituents have exerted highly potent activity. Thus, the title compounds represent novel class of potent antiglycating agents.
已经报道了甘氨酰/脯氨酰偶联苯并异噁唑的一系列新的脲/硫脲衍生物的合成。通过物理和光谱数据对化合物的结构进行了表征，并对其体外抗糖化活性进行了筛选。与标准芦丁（IC50=41.9μM）相比，几种化合物表现出有希望的活性，IC50<5μM。此外，发现含有甲氧基和溴取代基的化合物具有很强的活性。因此，标题化合物代表了一类新型的有效抗糖化剂。
